129798-93-2Relevant academic research and scientific papers
Synthesis and platelet-activating factor (PAF)-antagonistic activities of trisubstituted piperazine derivatives
Fukushi,Mabuchi,Terashita,Nishikawa,Sugihara
, p. 551 - 559 (1994)
2- or 3-Substituted 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclobepten-8- ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)- and 4-(3,4,5- trimethoxybenzyl)piperazines (2a - s, 3a, b) were prepared and evaluated for antagonistic activities against platelet-activating
Structure-activity relationships in platelet-activating factor. Part 13: Synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 or pure antiretroviral activity
Serradji, Nawal,Bensaid, Okkacha,Martin, Marc,Sallem, Wafa,Dereuddre-Bosquet, Nathalie,Benmehdi, Houcine,Redeuilh, Catherine,Lamouri, Aazdine,Dive, Georges,Clayette, Pascal,Heymans, Francoise
, p. 8109 - 8125 (2007/10/03)
HIV-1 infection of the brain and PAF neurotoxicity are implicated in AIDS dementia complex. We previously reported that a trisubstituted piperazine derivative is able to diminish both HIV-1 replication in monocyte-derived macrophages and PAF-induced platelet aggregation. We report in this work new compounds obtained by modifying its piperazine substituents. The structure-activity relationship study shows that a better dual activity or even pure antiretroviral compounds can be obtained in this series.
Trisubstituted piperazine compounds, their production and use
-
, (2008/06/13)
Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: STR1 wherein R1, R2 and R3 are lower alkyl groups; A is a phenyl group, a hydrocarbon group formed by condensation of two or three 5- to 8-membered rings, a monocyclic 5- to 8-membered heterocyclic group containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, a dicyclic heterocyclic group formed by condensation of a benzene ring with a 5- to 8-membered hetero-ring containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, a tricyclic heterocyclic group formed by condensation of (i) a 5- to 8-membered hetero-ring containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, and (ii) a benzene ring, and (iii) a benzene ring or a 5- to 8-membered hetero-ring containing 1 to 3 hetero-atoms selected from the class consisting of nitrogen, oxygen and sulfur, or a styryl group of the formula: Ar--CR4 =CR5 -- wherein Ar is a phenyl group, and R4 and R5 are independently hydrogen or a lower alkyl group, the phenyl group represented by A or Ar, the hydrocarbon group represented by A, the monocyclic 5- to 8-membered heterocyclic group represented by A, the dicyclic heterocyclic group represented by A and the tricyclic heterocyclic group represented by A being unsubstituted or substituted by one or more substituents selected from the class consisting of a lower alkyl group, a halo lower alkyl group, a hydroxy lower alkyl group, an acyloxy lower alkyl group, a lower alkoxy lower alkyl group, a lower alkoxy group, a halo lower alkoxy group, a lower alkoxycarbonyl lower alkoxy group, a lower alkenyloxy group, aralkyloxy group, a lower alkoxy lower alkoxy group, a lower alkoxycarbonyl group, carboxyl group, carbamoyl group, an N,N-di-lower alkylcarbamoyl group, an N-lower alkylcarbamoyl group, halo group, cyano group, nitro group, hydroxy group, acyloxy group, amino group, a lower alkylsulfonylamino group, acylamino group, a lower alkoxycarbonylamino group, acyl group, mercapto group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group and oxo group; X is methylene group, carbonyl group or thiocarbonyl group and G is a group of the formula: --CH2 --n Z--R6 wherein n is an integer of 0 to 2, Z is a chemical bond, O, S, SO, SO2, CO, COO, OCO, OCONR7, CONR7 or NR7 (wherein R7 is hydrogen, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group or a lower alkoxycarbonyl group), and R6 is hydrogen, a lower alkyl group, a lower haloalkyl group or a lower alkenyl group, provided that, when n is O and Z is chemical bond, R6 is not hydrogen or a lower alkyl group are useful as a platelet activating factor antagonist.
Trisubstituted piperazine compounds, their production and use
-
, (2008/06/13)
Novel trisubstituted piperazine compounds of the formula (I): wherein A is an optionally substituted phenyl group, an optionally substituted condensed polycyclic hydrocarbon group, an optionally substituted hetero-cyclic group or a styryl group of the formula:, Ar - CR4 = CR5 - wherein Ar is an optionally substituted phenyl group, and R4 and R5 are independently hydrogen or a lower alkyl group, X is methylene group, carbonyl group or thiocarbonyl group, G is a group of the formula:, nZ-R6 wherein n is an integer of 0 to 2, Z is a chemical bond, O, S, SO, SO2, CO, COO, CONR7 or NR7 (wherein R7 is hydrogen, a lower alkyl group, a lower haloalkyl group, a lower alkenyl group or a lower alkoxycarbonyl group), and R6 is hydrogen, a lower alkyl group, a lower haloalkyl group or a lower alkenyl group, provided that, when n is 0 and Z is chemical bond, R6 is not hydrogen or a lower alkyl group, and R1, R2 and R3 are independently a lower alkyl group, and salts thereof, are useful as a platelet activating factor antagonist.
